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Extended delivery of an anionic drug by contact lens loaded with a cationic surfactant.

Biomaterials (2013-01-23)
Lokendrakumar C Bengani, Anuj Chauhan
ABSTRACT

Drug eluding contact lenses can be very effective vehicles for ophthalmic drug delivery, but are incapable of releasing drug for more than a few hours. We propose to optimize the interactions of the polymer matrix of the contact lens with the hydrophobic tails of ionic surfactants to adsorb the surfactant molecules on the polymer with high packing and thus create a high surface charge. Ionic drugs can then adsorb on the charged surfactant coated surfaces with high affinity to reduce the transport rates, leading to extended release. Specifically, we show control release of an anionic drug dexamethasone 21-disodium phosphate from poly-hydroxyethyl methacrylate (p-HEMA) contact lenses by utilizing cationic surfactant (cetalkonium chloride). The partition coefficient of the drug increase exponentially with surfactant loading in the gel in at least qualitative agreement with the Debye-Hückel theory. The drug adsorbs on the surfactant covered polymer, and can also diffuse along the surface with diffusivity lower than that for the free drug, leading to a reduction in the effective diffusivity, which is the weighted combination of the free and surface diffusivities. The addition of surfactant did not impact transparency of lenses, and had additional benefits of increase in wettability and significant reduction in protein absorption. With a surfactant loading of about 10%, the drug release duration was increased from about 2 h to 50 h in 1-day ACUVUE(®) contact lenses, proving the viability of using surfactant for increasing drug release durations.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Dexamethasone 21-phosphate disodium salt, ≥98%
Sigma-Aldrich
2-Hydroxyethyl methacrylate, ≥99%, contains ≤50 ppm monomethyl ether hydroquinone as inhibitor
Sigma-Aldrich
2-Hydroxyethyl methacrylate, contains ≤250 ppm monomethyl ether hydroquinone as inhibitor, 97%
Sigma-Aldrich
2-Hydroxyethyl methacrylate, embedding medium (for microscopy)
Dexamethasone sodium phosphate, European Pharmacopoeia (EP) Reference Standard